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Cholinergics Flashcards

(50 cards)

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1
Q

Nicotinic Antagonist
Competitive Nn blocker

Use - lowers blood pressure
This drug was introduced in the 50’s and there are way better anti-hypertensives

A

MECAMYLAMINE

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2
Q

TACRINE, DONEPZIL, RIVASTIGMINE, GALANTAMINE

A

Long acting AChE-inhibitors used to treat DEMENTIA

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3
Q

BETHANACHOL

A

Half-life - long, not a substrate for acetylcholinesterase

Use - Nonobstructive GI Disorders or URINARY RETENTION

Stimulate GI motility and bladder emptying

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4
Q

d-Tubocurarine

A

Muscle relaxant
Active component in curare, hypotension
Rarely used due to tendency to release histamine and cause bronchospasm
Some cross reactivity with Nn

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5
Q

CARBACHOL

A

Half-life - long, not a substrate for acetylcholinesterase

Pupillary constriction
Use - limited, because nicotinic activity stimulates all autonomic ganglia

Some application in treating glaucoma

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6
Q

More selective for M1, which lessens side effects
Less tendency for dry mouth/blurred vision
Peptic Ulcer Disease - suppresses acid secretion via action on parietal cells

A

PIRENZIPINE

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7
Q

TIOTROPIUM

A

Bronchodilation

Supposedly more bronchoselective than ipratropium
Has less affinity for M2 receptors (doesn’t cause cardiac side effects)
Increase exercise tolerance

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8
Q

Spasmolytic

Stimulates presynaptic GABA-B receptors, suppressing excitatory transmissions

A

BACLOFEN

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9
Q

Similar to neostigmine but with a longer duration

MYASTHENIA GRAVIS — primary drug

A

PYRIDOSTIMINE

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10
Q

Inhibits calcium release from sarcoplasmic reticulum

Treat malignant hypertherima

A

DANTROLENE

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11
Q

Muscle relaxant
Active component in curare, hypotension
Rarely used due to tendency to release histamine and cause bronchospasm
Some cross reactivity with Nn

A

d-Tubocurarine

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12
Q

Chronic Asthma/COPD - induces bronchodilation but does not inhibit ciliary motility
Note for acute asthma attacks (beta-2 agonists are much better)
Rhinorrhea — stops runny nose

A

IPRATROPIUM

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13
Q

MECAMYLAMINE

A

Nicotinic Antagonist
Competitive Nn blocker

Use - lowers blood pressure
This drug was introduced in the 50’s and there are way better anti-hypertensives

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14
Q

ATROPINE

A

M1, M2, and M3 receptors
Eyes - causes MYDRIASIS & CYCLOPLEGIA
Promotes BRONCHODILATION and reduces secretions

Initial bradycardia, but in general causes TACHYCARDIA
TREAT AV-blocks and post-MI bradycardia

GI - antispasmodic, can be used to treat IBS

Use for OVERACTIVE BLADDER

Anti-AchE poisoning

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15
Q

BACLOFEN

A

Spasmolytic

Stimulates presynaptic GABA-B receptors, suppressing excitatory transmissions

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16
Q

PYRIDOSTIMINE

A

Similar to neostigmine but with a longer duration

MYASTHENIA GRAVIS — primary drug

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17
Q

TOLTERODINE, OXYBUTYNIN, DARIFENACIN, SOLIFENACIN

A

Slightly more selective for the M3 receptors
Used to treat OVERACTIVE BLADDER and incontinence
Neurologic problems

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18
Q

SUCCINYLCHOLINE

A 
Depolarizing blocker
Hyperkalemia
Myalgia 
Ganglionic Stimulation
Malignant Hyperthermia
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19
Q

Eyes - causes MYDRIASIS & CYCLOPLEGIA
Promotes BRONCHODILATION and reduces secretions

Initial bradycardia, but in general causes TACHYCARDIA
TREAT AV-blocks and post-MI bradycardia

GI - antispasmodic, can be used to treat IBS

Use for OVERACTIVE BLADDER

Anti-AchE poisoning

A

ATROPINE

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20
Q

Prophylactic for MOTION SICKNESS

Can be used as a patch

A

SCOPOLAMINE

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21
Q 
Depolarizing blocker
Hyperkalemia
Myalgia 
Ganglionic Stimulation
Malignant Hyperthermia
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A

SUCCINYLCHOLINE

22
Q

PIRENZIPINE

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A

More selective for M1, which lessens side effects
Less tendency for dry mouth/blurred vision
Peptic Ulcer Disease - suppresses acid secretion via action on parietal cells

23
Q

Partial nicotinic agonist that reduces nicotine craving

Causes nightmares

24
Q

Covalently bind and inactivate AChE, undergo aging (irreversible)

SLUDGEM symptoms - Bradycardic, Excessive Tearing, Can’t breathe

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A

Parathion, Malathion, Echothiophate

25
``` Use — DIAGNOSIS of myasthenia gravis via injection Cholinergic Crisis (Tensilon Test) - identify if they are OVER or UNDER treated ```
EDROPHONIUM
26
IPRATROPIUM
Chronic Asthma/COPD - induces bronchodilation but does not inhibit ciliary motility Note for acute asthma attacks (beta-2 agonists are much better) Rhinorrhea — stops runny nose
27
Anti-Cholinergic Toxicity
Hot dry skin, Dry mouth, Dry eyes Mydriasis and Cyclopegia —> Blurred vision (Blind as a bat) Narrowing of anterior chamber and diminished outflow of aqueous humor Sedation, Agitation, Hallucination, Coma (Mad as a Hatter)
28
PILOCARPINE
Half-life - long, not a substrate for acetylcholinesterase Glaucoma - contracts ciliary muscle and increases outflow of aqueous humor Xerostomia - stimulates salivary glands, useful in Sjorgen's syndrome Can cause Diaphoresis
29
GI atony - used in cases of post-operative paralysis of the GI tract GU atony - used in post-operative dysuria Glaucoma - miosis, lowers IOP Myasthenia Gravis - most common treatment in the US, increases Ach concentration @ NMJ NM blockade reversal - reverses paralysis from competitive NM blockade agents (eg Curare and related drugs)
NEOSTIGMINE
30
Act on GABA receptors in the CNS
DIAZEPAM
31
Long acting AChE-inhibitors used to treat DEMENTIA
TACRINE, DONEPZIL, RIVASTIGMINE, GALANTAMINE
32
Half-life - long, not a substrate for acetylcholinesterase Use - Nonobstructive GI Disorders or URINARY RETENTION Stimulate GI motility and bladder emptying
BETHANACHOL
33
Slightly more selective for the M3 receptors Used to treat OVERACTIVE BLADDER and incontinence Neurologic problems
TOLTERODINE, OXYBUTYNIN, DARIFENACIN, SOLIFENACIN
34
METHACHOLINE
No effect in normal patients, but will provoke airway constriction in asthmatics Used to diagnose bronchial hyperreactivity (asthma) WHEEZING
35
SCOPOLAMINE
Prophylactic for MOTION SICKNESS | Can be used as a patch
36
No effect in normal patients, but will provoke airway constriction in asthmatics Used to diagnose bronchial hyperreactivity (asthma) WHEEZING
METHACHOLINE
37
EDROPHONIUM
``` Use — DIAGNOSIS of myasthenia gravis via injection Cholinergic Crisis (Tensilon Test) - identify if they are OVER or UNDER treated ```
38
Parathion, Malathion, Echothiophate
Organophosphates Covalently bind and inactivate AChE, undergo aging (irreversible) SLUDGEM symptoms - Bradycardic, Excessive Tearing, Can’t breathe Tx: Pralidoximine, Atropine
39
Half-life - long, not a substrate for acetylcholinesterase Glaucoma - contracts ciliary muscle and increases outflow of aqueous humor Xerostomia - stimulates salivary glands, useful in Sjorgen's syndrome Can cause Diaphoresis
PILOCARPINE
40
Bronchodilation Has less affinity for M2 receptors (doesn't cause cardiac side effects) Increase exercise tolerance
TIOTROPIUM
41
VARENCICLINE ("Chantix")
Partial nicotinic agonist that reduces nicotine craving Causes nightmares 1-800-VERY CLEAN
42
Sometimes used in ophthalmic surgery to constrict pupil (Miochol)
Acetylcholine
43
Acetylcholine
Half-life - very short, rapidly metabolized by acetylcholinesterase Use - Limited clinical use due to potential side effects, sometimes used in ophthalmic surgery to constrict pupil (Miochol)
44
NEOSTIGMINE
GI atony - used in cases of post-operative paralysis of the GI tract GU atony - used in post-operative dysuria Glaucoma - miosis, lowers IOP Myasthenia Gravis - most common treatment in the US, increases Ach concentration @ NMJ NM blockade reversal - reverses paralysis from competitive NM blockade agents (eg Curare and related drugs)
45
DIAZEPAM
Spasmolytic | Benzodiazepines act on GABA receptors in the CNS
46
Rocuronium
Muscle relaxant for surgery | Nm selective, no CV side effects
47
Muscle relaxant for surgery | Nm selective, no CV side effects
Rocuronium
48
DANTROLENE
Inhibits calcium release from sarcoplasmic reticulum | Treat malignant hyperthermia
49
Half-life - long, not a substrate for acetylcholinesterase Pupillary constriction Use - limited, because nicotinic activity stimulates all autonomic ganglia Some application in treating glaucoma
CARBACHOL
50
Hot dry skin, Dry mouth, Dry eyes Mydriasis and Cyclopegia —> Blurred vision (Blind as a bat) Narrowing of anterior chamber and diminished outflow of aqueous humor Sedation, Agitation, Hallucination, Coma (Mad as a Hatter)
Anti-Cholinergic Toxicity

Pharmacology (19 decks)

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